| 名称 | Paquinimod |
| 描述 | Paquinimod (ABR 25757) is a specific S100A8/S100A9 inhibitor with oral activity. Paquinimod has immunomodulatory activity and can be used for the treatment of systemic lupus erythematosus. |
| 动物实验 | Two OA mouse models differing in level of synovial activation were treated prophylactic with paquinimod. Synovial thickening, osteophyte size and cartilage damage were measured histologically, using an arbitrary score, adapted Pritzker OARSI score or imaging software, respectively. Human OA synovia were stimulated with S100A9, with or without paquinimod[1].Seven weeks old female B6.Cg-Fbn1(Tsk)/J (Tsk-1) mice were treated with vehicle or paquinimod at the dose of 5 or 25mg/kg/day in the drinking water for 8 weeks. The effect of paquinimod on the level of skin fibrosis and on different subpopulations within the myeloid cell compartment in skin biopsies were evaluated by using histology, immunohistochemisty, a hydroxyproline assay and real-time PCR. Furthermore, the level of IgG in serum from treated animals was also analysed. The statistical analyses were performed using Mann-Whitney nonparametric two tailed rank test[1]. |
| 体内活性 | 方法：为检测对中性粒细胞哮喘小鼠模型的影响，将 Paquinimod (0.1-25 mg/kg) 饮用水口服给药给 OVA/CFA 致敏和激发的 C57BL/6 小鼠，每天一次，持续十七天。
结果：Paquinimod 可能通过下调 IL-17、IFN-γ 和 IL-1β，有效抑制中性粒细胞哮喘小鼠模型中的中性粒细胞炎症和重塑。[1]
方法：为检测抗炎活性，将 Paquinimod (-25 mg/kg) 饮用水口服给药给 NOD 炎症性纤维化 (N-IF) 小鼠，每天一次，持续 4-10 周。
结果：使在疾病发作后开始治疗，对 N-IF 小鼠的治疗也能显著减少炎症并导致纤维化消退。疾病表型的减少与促进疾病的转基因 NKT-II 细胞及其 2-型细胞因子表达谱的数量和活化的系统性减少有关。[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (142.69 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 12.5 mg/mL (35.67 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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| 关键字 | Inhibitor | inhibit | ABR25757 | ABR-25757 | Paquinimod |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | ReFRAME 相关化合物库 | NO PAINS 化合物库 | 抗病毒库 | 临床期小分子药物库 | 药物功能重定位化合物库 | 人代谢物化合物库 |
